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Dasatinib

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产品编号 T1448Cas号 302962-49-8
别名 达沙替尼, BMS-354825

Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂,抑制 Src 和 Bcr-Abl (Ki=16/30 pM),具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性,用于治疗白血病和淋巴瘤等。

Dasatinib

Dasatinib

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纯度: 99.89%
产品编号 T1448 别名 达沙替尼, BMS-354825Cas号 302962-49-8

Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂,抑制 Src 和 Bcr-Abl (Ki=16/30 pM),具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性,用于治疗白血病和淋巴瘤等。

规格价格库存数量
5 mg¥ 153现货
10 mg¥ 198现货
25 mg¥ 318现货
50 mg¥ 453现货
100 mg¥ 656现货
200 mg¥ 958现货
500 mg¥ 1,580现货
1 mL x 10 mM (in DMSO)¥ 152现货
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产品介绍

生物活性
产品描述
Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.
靶点活性
Abl:0.6 nM (cell free), c-Kit (D816V):37 nM (cell free), c-Kit (WT):79 nM (cell free), Src:0.8 nM (cell free)
体外活性
方法:8 种甲状腺癌细胞用 Dasatinib (0.019-1.25 μmol/L) 处理 3 天,使用 SRB 方法检测细胞增殖。
结果:Dasatinib 对 C643、TPC1、BCPAP、SW1736、K1、8505C、HTh74、HTh7 细胞的 IC50 分别为 0.09、0.03、0.04、0.08、0.4、2.7、>5、1.6 μmol/L。[1]
方法:人肺癌细胞 NCI-H1975 和 NCI-H1650 用 Dasatinib (2.5-20 μM) 处理 48 h,使用 Flow Cytometry 检测细胞凋亡情况。
结果:Dasatinib 在 10 和 20 μM 下诱导 NCI-H1975 和 NCI-H1650 细胞凋亡。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Dasatinib (50 mg/kg in 80 mmol/L sodium citrate buffer, pH 3.0) 口服给药给携带人甲状腺癌肿瘤 BCPAP 或 8505C 的 athymic nude 小鼠,每周五天,持续二十天。
结果:Dasatinib 显著抑制 BCPAP 原位肿瘤,最终肿瘤体积抑制了 90% 以上。Dasatinib 治疗在任何时间点都没有显著抑制 8505C 来源的肿瘤的生长。[1]
方法:为研究对神经炎症的影响,将 Dasatinib (20 mg/kg in 4%DMSO+30%PEG+5%Tween 80) 腹腔注射或口服给药给 C57BL6/N 小鼠,每天一次给药四天,随后腹腔注射 LPS (10  mg/kg) 诱导体内神经炎症反应。
结果:腹腔注射和口服 Dasatinib 抑制 LPS 诱导的野生型小鼠脑中小胶质细胞/星形胶质细胞活化、促炎细胞因子水平和中性粒细胞滚动。[3]
激酶实验
Kinase assays using wild-type and mutant glutathione S-transferase (GST)–Abl fusion proteins (c-Abl amino acids 220-498) were done as described, with minor alterations. GST-Abl fusion proteins were released from glutathione-Sepharose beads before use; the concentration of ATP was 5 μmol/L. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins were treated with LAR tyrosine phosphatase according to the manufacturer's instructions. After 1-hour incubation at 30°C, LAR phosphatase was inactivated by addition of sodium vanadate (1 mmol/L). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase was routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations were 0 to 5,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The BMS-354825 concentration range was extended to 1,000 nmol/L for mutant T315I. These same inhibitor concentrations were used for the in vitro peptide substrate phosphorylation assays. The three inhibitors were tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase [1].
细胞实验
Ba/F3 cell lines were plated in triplicate and incubated with escalating concentrations of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90 determinations were 0 to 2,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The imatinib concentration range was extended to 6,400 nmol/L for mutants with IC50 >2,000 nmol/L. The BMS-354825 concentration range was extended to 200 nmol/L for mutant T315I [1].
动物实验
For in vivo studies, dasatinib (50 mg/kg) was prepared for daily oral gavage (5 d/wk) in 80 mmol/L sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice were randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice received dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment) [4].
别名达沙替尼, BMS-354825
化学信息
分子量488.01
分子式C22H26ClN7O2S
CAS No.302962-49-8
SmilesN(C1=CC(N2CCN(CCO)CC2)=NC(C)=N1)C=3SC(C(NC4=C(C)C=CC=C4Cl)=O)=CN3
密度1.408g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9.1 mg/mL (18.65 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 55 mg/mL (112.7 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.0491 mL10.2457 mL20.4914 mL102.4569 mL
5 mM0.4098 mL2.0491 mL4.0983 mL20.4914 mL
10 mM0.2049 mL1.0246 mL2.0491 mL10.2457 mL
1mg5mg10mg50mg
20 mM0.1025 mL0.5123 mL1.0246 mL5.1228 mL
50 mM0.0410 mL0.2049 mL0.4098 mL2.0491 mL
100 mM0.0205 mL0.1025 mL0.2049 mL1.0246 mL

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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